预约演示
更新于：2026-03-20
Tirapazamine
替拉扎明
更新于：2026-03-20
概要
基本信息
非在研机构 |
权益机构- |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床2/3期 |
特殊审评孤儿药 (美国)、孤儿药 (欧盟) |
登录后查看时间轴
结构/序列
分子式C7H6N4O2 |
InChIKeyORYDPOVDJJZGHQ-UHFFFAOYSA-N |
CAS号27314-97-2 |
关联
19
项与 替拉扎明 相关的临床试验NCT06844357
A Multi-center, Randomized, Controlled, Open-label Phase II/III Clinical Trial to Investigate Whether Transarterial Tirapazamine Injection Followed by Transarterial Embolization (TATE) is Superior to Traditional Transarterial Chemoembolization (TACE) in Patients With Intermediate-Stage Hepatocellular Carcinoma (HCC)
NCT06848556
A Multicenter, Randomized, Controlled, Open-label Phase I/II Study to Evaluate the Pharmacokinetics of Transarterial Tirapazamine Embolization for Intermediate-stage Hepatocellular Carcinoma, and Compare Its Efficacy and Safety with Transarterial Chemoembolization
NCT03145558
TATE Versus TACE, an Open-label Randomized Study Comparing TransArterial Tirapazamine Embolization Versus TransArterial ChemoEmbolization in Intermediate Stage Hepatocellular Carcinoma
100 项与 替拉扎明 相关的临床结果
登录后查看更多信息
100 项与 替拉扎明 相关的转化医学
登录后查看更多信息
100 项与 替拉扎明 相关的专利（医药）
登录后查看更多信息
619
项与 替拉扎明 相关的文献（医药）2025-10-01JOURNAL OF COLLOID AND INTERFACE SCIENCE
Engineering hypoxia-specific core–shell nanotherapeutics: A sequential strategy for amplified multimodal synergistic breast cancer treatment
Article
作者: Wang, Yuqing ; Qin, Siyong ; Liu, Wenlong ; Liu, Muhai ; Zeng, Fangyu ; Liu, Qiangyu ; Mo, Qin ; Ma, Yihan ; Zhang, Aiqing ; Cheng, Yinjia ; Li, Yuting ; Zhang, Xianzheng
The reactive oxygen species (ROS)-based chemodynamic therapy (CDT) and sonodynamic therapy (SDT) have garnered significant interests in advanced tumor treatments. However, their therapeutic efficacy is severely hindered by tumor hypoxia and overexpressed antioxidant glutathione (GSH) in the tumor microenvironment (TME). Motivated by the concept of metal coordination-based nanomedicine, we proposed an innovative strategy for synergistic tumor therapy tailored to the TME. Herein, we developed a multifunctional targeted delivery nanosystem based on the tirapazamine (TPZ)-loaded BT@M/T@T(Cu)GH cascade nanoreactor to enhance the synergistic efficacy of CDT, SDT, chemotherapy (CT) and starvation therapy (ST) against breast cancer. The rationally designed nanoreactor was constructed through covalent conjugation of glucose oxidase (GOx) onto TPZ-loaded BT@M/T@T(Cu) nanoparticles, wherein the formed tannic acid/copper (Ⅱ) (T(Cu)) network served as the "nanovalve"for BT@M/T nanoparticles. Surface functionalization with hyaluronic acid (HA) enabled BT@M/T@T(Cu) nanoparticles to effectively target CD44-overexpressed 4T1 breast tumors via passive targeting and active targeting effect, while mitigating cytotoxicity toward normal cells/tissues. Following successful tumor accumulation, BT@M/T@T(Cu)GH nanoparticles underwent pH-dependent disassembly and released TPZ, Cu2+ and GOx, initiating a cascade of integrated therapeutic functions, including redox balance disruption, starvation, oxidative cytotoxicity, and hypoxia-activated chemotoxicity. When exposed to ultrasound (US) irradiation, BT@M/T@T(Cu)GH nanoparticles demonstrated sonosensitization capability, generating substantial singlet oxygen (1O2) through energy transfer processes. Owing to all these prominent features, the all-in-one nanomedicine exhibited significant apoptotic cell death and noteworthy tumor eradication in vivo, via synergistic combination of GOx-based ST, self-amplified CDT, hypoxia-activated CT, and US-activated SDT. Additionally, the administration of BT@M/T@T(Cu)GH had negligible effects on the normal growth. Taken together, this work establishes a versatile TiO2-based nanosystem integrating tumor targeting and multi-mode synergistic therapy of breast cancer, offering a novel strategy for highly effective and precise treatment of malignancies.
2025-05-01CHEMICAL ENGINEERING JOURNAL
A vascular heterogeneity-orienting TACE strategy addresses peripheral tumor and avascular deep tumor for complete hepatocellular carcinoma clearance
作者: Yu, Meng ; Li, Shuping ; Tang, Yuhao ; Chen, Jinbin ; Peng, Zhenwei ; Mei, Jie ; Peng, Wei ; Wei, Guangyan ; Zhu, Meiyan ; Xu, Li ; Quan, Xiaolong
Transcatheter arterial chemoembolization (TACE) is considered a frontline therapeutic strategy for intermediate-stage and advanced hepatocellular carcinoma (HCC) through selective embolization of tumor-feeding vessels.However, the exacerbation of hypoxic conditions, along with inefficient drug transport through the bloodstream in residual tumor tissues contributes to poor prognosis after TACE.This study improved the conventional TACE treatment by developing a photothermal-triggered TACE embolization agent (MPMT@Gel), comprising photothermal metal-polyphenol nanocarrier, which loaded with hypoxia-activated chemotherapeutic drug tirapazamine (TPZ) and decorated with penetration enhancer menthol on the surface to serve as photo-controlled release gatekeeper.The MPMT@Gel was activated by near-IR light not only to harness the photothermal-enhanced embolization effect in the xenografted HCC vasculature (p < 0.001), but also to induce the self-feedback cytotoxicity by releasing and distributing the TPZ within hypoxic tumor tissues in response to photothermal stimulation (cell mortality rate of 6.07% to 85.13%).Furthermore, we firstly found that menthol could inhibit tumor angiogenesis (reduced 71.4%) and lung metastasis via reducing EGFR expression (reduced 66.9%).This strategy was demonstrated for the first time on orthotopic HCC mouse model, simultaneously eliminating vascularized peripheral tumor and avascular deep tumor, preventing residual tissue recurrence (HR 0.003; p = 0.004) and lung metastasis (reduced 100%).These findings highlight the great clin. potential of this innovative TACE approach.
2025-05-01Small
Synergistic Comprehensive Activation Methods for Dual‐Modality PDT and Hypoxia‐Triggered Chemotherapy Guided by NIR‐II Imaging beyond 1700 nm in Deep Tumors
Article
作者: Gan, Dechao ; Liu, Shengnan ; Kong, Xianggui ; Li, Dabing ; Li, Qiqing ; Li, Xiaodan ; Chang, Yulei ; Chen, Haoran ; Wang, Wang ; Long, Fei ; Li, Bin
Abstract:
Although photodynamic therapy (PDT) holds great promise for applications in cancer treatment, it has limited effectiveness against deep hypoxic tumors. Moreover, the lack of visualization guidance for precision theranostics poses additional challenges, hindering its broader clinical adoption. By combining NIR‐IIc (1800 nm) imaging guidance with internally and externally activatable dual‐modality PDT and hypoxia‐triggered chemotherapy, this study proposes a conceptual framework to overcome these limitations. This approach involves the use of photoswitchable lanthanide‐doped nanoparticles featuring Tm3+‐activated upconversion/downshifting emissions coupled with carboxyl‐terminated Ir(III) complex‐based Type I/II photosensitizer to form a nanophotosensitizer. The findings demonstrate that this system enabled NIR‐IIc imaging guidance upon 808/980 nm excitation while selectively activating external PDT under 980 nm irradiation, thereby ensuring accurate therapy and minimizing phototoxicity risk. The Ir(III) complex conjugates with luminol to form a self‐illuminating Type I/II photosensitizer, which can respond to the elevated H2O2 levels in the tumor microenvironment, effectively catalyzing chemiluminescence‐assisted PDT. Moreover, PDT aggravates tumor hypoxia, which in turn activates the hypoxia‐activatable prodrugs like tirapazamine, resulting in a synergistic antitumor effect. With NIR‐IIc imaging‐guided dual‐modality PDT, this study introduces a groundbreaking approach that unites Type I/II PDT with chemotherapy, significantly advancing the precise and effective treatment of deep hypoxic tumors.
100 项与 替拉扎明 相关的药物交易
登录后查看更多信息
研发状态
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 肝细胞癌 | 临床3期 | 中国 | 2025-03-11 | |
| 宫颈癌 | 临床3期 | 美国 | 2014-07-28 | |
| 头颈部鳞状细胞癌 | 临床3期 | 美国 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 阿根廷 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 澳大利亚 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 加拿大 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 智利 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 法国 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 德国 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 中国香港 | 2005-04-01 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1/2期 | 17 | 鹹積鏇構繭餘繭範積鏇(窪艱製窪齋醖築壓鹽淵) = 鏇艱簾鏇糧醖膚範積醖 憲網顧顧窪壓顧淵獵鏇 (膚膚醖壓齋窪壓齋糧觸 ) 更多 | 积极 | 2022-06-21 | |||
临床1期 | 27 | 積範壓鏇觸餘鹽餘膚淵(鑰壓願願鏇糧蓋衊鑰鏇) = hypertension and transient elevation of AST/ALT in 70.4% 觸壓網窪艱鹽襯鏇繭廠 (鬱鬱顧蓋廠齋廠觸製窪 ) 更多 | 积极 | 2021-05-17 | |||
临床3期 | 402 | (Concurrent Cisplatin and Radiation) | 襯糧糧鹹製壓糧構鏇製 = 鬱選醖鹹鏇鏇選鬱鬱築 鏇範壓醖襯觸醖鑰選獵 (艱鏇淵鏇獵鹽齋衊製鬱, 範餘構鬱顧遞餘衊醖觸 ~ 廠獵襯鹹醖餘網糧鏇齋) 更多 | - | 2017-07-02 | ||
(Concurrent Cisplatin, Tirapazamine and Radiation) | 襯糧糧鹹製壓糧構鏇製 = 窪窪糧構鏇廠積獵網築 鏇範壓醖襯觸醖鑰選獵 (艱鏇淵鏇獵鹽齋衊製鬱, 壓範膚獵餘壓顧餘獵願 ~ 憲襯積鬱觸醖廠範壓鑰) 更多 | ||||||
临床3期 | 861 | 鏇蓋淵簾遞憲窪鑰觸觸(壓網簾夢鬱繭範膚願鹹) = 鏇網窪襯鬱餘憲蓋壓鬱 鬱網遞餘遞窪鬱淵廠積 (膚壓夢顧糧顧窪繭蓋鏇 ) | 不佳 | 2009-11-01 | |||
鏇蓋淵簾遞憲窪鑰觸觸(壓網簾夢鬱繭範膚願鹹) = 願製壓膚網顧艱壓構憲 鬱網遞餘遞窪鬱淵廠積 (膚壓夢顧糧顧窪繭蓋鏇 ) | |||||||
N/A | 83 | 築餘鏇鬱鏇範簾醖糧淵(鬱廠鬱鬱積鹽蓋夢遞顧) = 觸範壓衊醖顧襯鹽鏇觸 膚蓋夢醖獵衊願願選積 (網觸醖顧糧夢築繭廠夢 ) 更多 | - | 2008-05-20 | |||
临床2期 | 小细胞肺癌 巩固 | 69 | Tirapazamine (TPZ)/cisplatin/etoposide (PE) and concurrent thoracic radiotherapy (TRT) | 鏇鏇鏇衊觸艱窪鏇築齋(構獵繭鑰廠膚蓋鑰襯齋) = 鹽簾鑰糧鏇廠窪獵構廠 鏇憲淵獵繭觸廠蓋簾憲 (襯蓋顧壓範膚壓壓壓蓋 ) 更多 | - | 2008-05-20 | |
临床1期 | 11 | 顧鹹襯構蓋糧範鹹鏇鑰(糧壓鏇夢窪窪糧膚夢壓) = 艱鹽衊壓蓋壓鑰網廠醖 淵窪衊齋顧壓鬱憲選醖 (齋願膚鏇鹽糧製網願構 ) 更多 | - | 2007-06-20 | |||
临床2期 | 63 | TPZ arm | 齋淵廠艱積艱膚鑰鏇顧(淵醖積膚壓鏇觸範膚構) = 構廠繭艱鏇蓋艱襯鹽憲 淵遞鑰鏇鏇窪夢遞選積 (顧範襯鑰艱範餘繭願繭 ) 更多 | - | 2006-05-01 | ||
临床2期 | 65 | 窪夢積顧憲選構範鏇構(醖憲網築蓋夢鏇積醖積) = frequent constitutional (23%) grade 3 or 4 toxicity 築鹹鏇蓋膚遞遞鹹積衊 (齋鏇選築淵願鏇餘鬱獵 ) 更多 | 积极 | 2006-03-01 | |||
N/A | 56 | 顧糧醖遞衊築鏇遞製顧(觸製夢鏇獵鹽網獵鬱鬱) = three cases 醖廠鹹蓋觸糧簾構構醖 (構積築淵顧糧選願鹹繭 ) 更多 | - | 2006-01-01 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
生物医药百科问答
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用